ASIA unversity:Item 310904400/113030
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    题名: Caffeic Acid Attenuates Multi-Drug Resistance in Cancer Cells by Inhibiting Efflux Function of Human P-glycoprotein
    作者: Teng, Yu-Ning
    Teng, Yu-Ning
    王昭能
    Wang, Charles C.N.
    Li, Wei-Chieh
    Liao, Wei-Chieh
    Chin-Chuan, H
    Hung, Chin-Chuan
    贡献者: 生物資訊與醫學工程學系
    关键词: caffeic acid;cancer multidrug resistance;P-glycoprotein;phenolic acid
    日期: 2020-01-20
    上传时间: 2020-10-14 05:37:25 (UTC+0)
    出版者: 亞洲大學
    摘要: Multidrug resistance (MDR) is a complicated ever-changing problem in cancer treatment, and P-glycoprotein (P-gp), a drug efflux pump, is regarded as the major cause. In the way of developing P-gp inhibitors, natural products such as phenolic acids have gotten a lot of attention recently. The aim of the present study was to investigate the modulating effects and mechanisms of caffeic acid on human P-gp, as well as the attenuating ability on cancer MDR. Calcein-AM, rhodamine123, and doxorubicin were used to analyze the interaction between caffeic acid and P-gp, and the ATPase activity of P-gp was evaluated as well. Resistance reversing effects were revealed by SRB and cell cycle assay. The results indicated that caffeic acid uncompetitively inhibited rhodamine123 efflux and competitively inhibited doxorubicin efflux. In terms of P-gp ATPase activity, caffeic acid exhibited stimulation in both basal and verapamil-stimulated activity. The combination of chemo drugs and caffeic acid resulted in decreased IC50 in ABCB1/Flp-InTM-293 and KB/VIN, indicating that the resistance was reversed. Results of molecular docking suggested that caffeic acid bound to P-gp through GLU74 and TRY117 residues. The present study demonstrated that caffeic acid is a promising candidate for P-gp inhibition and cancer MDR attenuation.
    關聯: MACROMOLECULES
    显示于类别:[生物資訊與醫學工程學系 ] 期刊論文

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